Searches / Scientia Pharmaceutica[JOURNAL]

Scientia Pharmaceutica[JOURNAL]

Sun 200 papers
RSS

In Vitro Antimicrobial Activity of Gel Containing the Herbal Ball Extract against Propionibacterium acnes.

Jantarat C, Sirathanarun P, Chuchue T … +3 more , Konpian A, Sukkua G, Wongprasert P

Sci Pharm · 2018 Feb · PMID 29495650 · Full text

The herbal ball has been used as a Thai traditional medicine for relieving many diseases including acne. However, the application process of the herbal ball in practice is complicated and time consuming. The objective of... The herbal ball has been used as a Thai traditional medicine for relieving many diseases including acne. However, the application process of the herbal ball in practice is complicated and time consuming. The objective of this work was to utilize an herbal ball extract to formulate a gel to reach a more favorable use of the herbal ball for acne treatment. An herbal ball consisting of , , the Benchalokawichian remedy and the stem bark powder of was prepared. The obtained herbal ball was steamed and squeezed to obtain the extract. Gel formulations containing the herbal ball extract at concentrations of 0.1, 1 and 5% / were prepared based on a carbomer gel. The herbal ball extract had antioxidant (EC = 219.27 ± 36.98 μg/mL) and anti activities (minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) = 31.25 μg/mL). The 5% / gel formulation had antimicrobial activity against , showing an inhibition zone value of 10.00 ± 1.00 mm. This indicates that the developed gel formulation has potential for acne treatment. In comparison to the traditional method of herbal ball usage, the application of herbal ball extract in the form of gel should be more convenient to use.

UHPLC-UV Method for Simultaneous Determination of Perindopril Arginine and Indapamide Hemihydrate in Combined Dosage Form: A Stability-Indicating Assay Method.

Al-Tannak NF

Sci Pharm · 2018 Feb · PMID 29470453 · Full text

Perindopril arginine and Indapamide hemihydrate in combination were proven to have a synergistic antihypertensive impact when compared with the use of each component alone. Therefore, a new Ultra-High Performance Liquid... Perindopril arginine and Indapamide hemihydrate in combination were proven to have a synergistic antihypertensive impact when compared with the use of each component alone. Therefore, a new Ultra-High Performance Liquid Chromatography coupled with Ultraviolet detector (UHPLC-UV) method has been developed and subsequently validated for simultaneous determination of the anti-hypertensive combination of Perindopril arginine and Indapamide hemihydrate. The separation of Perindopril arginine and Indapamide hemihydrate was achieved using a BEH C18 (1.7 μm, 2.1 × 50 mm) analytical column (Waters Acquity UPLC) and a mobile phase composed of 0.01% v/v formic acid in water adjusted to pH 4 with acetic acid and acetonitrile (40:60 v/v). The method was able to separate Perindopril arginine and Indapamide hemihydrate within less than 4.5 min with high accuracy, precision, resolution, and sensitivity. The content of Perindopril arginine and Indapamide hemihydrate present in the dosage form Coversyl Plus (5000 µg of Perindopril arginine/1250 µg of Indapamide hemihydrate) was determined in triplicate to give a concentration of 4991 µg and 1247 µg, respectively, from the manufacturer's stated amounts with Relative Standard Deviation (%RSD) of ±0.63% for Perindopril arginine and ±0.84% for Indapamide hemihydrate. Moreover, the degradation products of the combination were elucidated by UHPLC-Quadrupole Time of Flight-Mass spectrometry (UHPLC-QToF-MS) under acidic, basic, and thermal conditions. In conclusion the developed UHPLC-UV method was sensitive, rapid, and precise. Furthermore, forced degradation studies were performed and the degradants were identified by UHPLC-Electro-Spray Ionization-QToF (UHPLC-ESI-QToF).

Effect of Apium graveolens Extract Administration on the Pharmacokinetics of Captopril in the Plasma of Rats.

Siska S, Mun Im A, Bahtiar A … +1 more , Suyatna FD

Sci Pharm · 2018 Feb · PMID 29462958 · Full text

(celery) is an edible and traditionally medicinal plant that is used worldwide, among others for the treatment of hypertension. Combining celery with antihypertensive drugs can affect the pharmacodynamics and pharmacokin... (celery) is an edible and traditionally medicinal plant that is used worldwide, among others for the treatment of hypertension. Combining celery with antihypertensive drugs can affect the pharmacodynamics and pharmacokinetics of the latter drugs. The aim of the study is to assess the effects of administrating the celery extract on captopril pharmacokinetics. Sprague-Dawley strain rats were divided into two groups ( = 6). Group I was given captopril (10 mg/kg Body Weight (BW)) orally, while Group II was pretreated with celery extract orally (40 mg/kg BW) an hour before administration of captopril. The blood samples were withdrawn at various intervals after drug administration. The captopril concentration was determined using liquid chromatography-mass spectrometry (LC-MS/MS) and from the blood data, the values of , , , , and area under the curve () were calculated. The results showed that oral administration of the celery extract increased (38.67%), (37.84%), and (58.10%) and decreased (27.45%) of captopril in Group II (celery + captopril) compared with Group I (captopril). In conclusion, celery extract can alter the pharmacokinetic of captopril when given in combination. The combination might be beneficial for the treatment of hypertension, as celery causes an increase in the plasma level of captopril, which can enhance its efficacy.

Theoretical and Experimental Studies on Inclusion Complexes of Pinostrobin and β-Cyclodextrins.

Kicuntod J, Sangpheak K, Mueller M … +8 more , Wolschann P, Viernstein H, Yanaka S, Kato K, Chavasiri W, Pongsawasdi P, Kungwan N, Rungrotmongkol T

Sci Pharm · 2018 Jan · PMID 29385698 · Full text

Pinostrobin (PNS) belongs to the flavanone subclass of flavonoids which shows several biological activities such as anti-inflammatory, anti-cancerogenic, anti-viral and anti-oxidative effects. Similar to other flavonoids... Pinostrobin (PNS) belongs to the flavanone subclass of flavonoids which shows several biological activities such as anti-inflammatory, anti-cancerogenic, anti-viral and anti-oxidative effects. Similar to other flavonoids, PNS has a quite low water solubility. The purpose of this work is to improve the solubility and the biological activities of PNS by forming inclusion complexes with β-cyclodextrin (βCD) and its derivatives, heptakis-(2,6-di--methyl)-β-cyclodextrin (2,6-DMβCD) and (2-hydroxypropyl)-β-cyclodextrin (HPβCD). The A-type diagram of the phase solubility studies of PNS exhibited the formed inclusion complexes with the 1:1 molar ratio. Inclusion complexes were prepared by the freeze-drying method and were characterized by differential scanning calorimetry (DSC). Two-dimensional nuclear magnetic resonance (2D-NMR) and steered molecular dynamics (SMD) simulation revealed two different binding modes of PNS, i.e., its phenyl- (-PNS) and chromone- (-PNS) rings preferably inserted into the cavity of βCD derivatives whilst only one orientation of PNS, where the -PNS ring is inside the cavity, was detected in the case of the parental βCD. All PNS/βCDs complexes had a higher dissolution rate than free PNS. Both PNS and its complexes significantly exerted a lowering effect on the IL-6 secretion in LPS-stimulated macrophages and showed a moderate cytotoxic effect against MCF-7 and HeLa cancer cell lines in vitro.

In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide.

Haltner-Ukomadu E, Gureyeva S, Burmaka O … +4 more , Goy A, Mueller L, Kostyuk G, Margitich V

Sci Pharm · 2018 Jan · PMID 29324660 · Full text

An investigation into the biopharmaceutics classification and a study of the in vitro bioavailability (permeability and solubility) of the antiviral compound enisamium iodide (4-(benzylcarbamoyl)-1-methylpyridinium iodid... An investigation into the biopharmaceutics classification and a study of the in vitro bioavailability (permeability and solubility) of the antiviral compound enisamium iodide (4-(benzylcarbamoyl)-1-methylpyridinium iodide) were carried out. The solubility of enisamium iodide was determined in four different buffers. Apparent intestinal permeability () of enisamium iodide was assessed using human colon carcinoma (Caco-2) cells at three concentrations. The solubility of enisamium iodide in four buffer solutions from pH 1.2 to 7.5 is about 60 mg/mL at 25 °C, and ranges from 130 to 150 mg/mL at 37 °C, depending on the pH. Based on these results, enisamium iodide can be classified as highly soluble. Enisamium iodide demonstrated low permeability in Caco-2 experiments in all tested concentrations of 10-100 μM with permeability coefficients between 0.2 × 10 cm s and 0.3 × 10 cm s. These results indicate that enisamium iodide belongs to class III of the Biopharmaceutics Classification System (BCS) due to its high solubility and low permeability. The bioavailability of enisamium iodide needs to be confirmed in animal and human studies.

4,5-Dimethoxy-2-nitrobenzohydrazides and 1-(1-Benzylpiperidin-4-yl)ethan-1-ones as Potential Antioxidant/Cholinergic Endowed Small Molecule Leads.

Banu R, Gerding J, Franklin C … +7 more , Sikazwe D, Horton W, Török M, Davis J, Cheng KH, Nakazwe M, Mochona B

Sci Pharm · 2017 Dec · PMID 29267246 · Full text

The objective of this research is to generate leads for developing our ultimate molecules with utility in central nervous system (CNS) diseases. Indeed, poly-active molecules capable of mitigating brain free radical dam... The objective of this research is to generate leads for developing our ultimate molecules with utility in central nervous system (CNS) diseases. Indeed, poly-active molecules capable of mitigating brain free radical damage while enhancing acetylcholine signaling (via cholinesterase inhibition) are still being sought for combating Alzheimer's disease (AD). We differentiate "poly-active" agents from "multi-target" ones by defining them as single molecular entities designed to target only specific contributory synergistic pharmacologies in a disease. For instance, in AD, free radicals either initiate or act in synergy with other pharmacologies, leading to disease worsening. For this preliminary report, a total of 14 (i.e., 4,5-dimethoxy-2-nitrobenzohydrazide plus 1-(1-benzylpiperidin-4-yl)ethan-1-one) derivatives were synthesized and screened, in silico and in vitro, for their ability to scavenge free radicals and inhibit acetylcholinesterase (AChE)/butyrylcholinesterase (BuChE) enzymes. Overall, six derivatives (, , , , , ) exhibited potent (>30%) antioxidant properties in the oxygen radical absorbance capacity (ORAC) assay. The antioxidant values were either comparable or more potent than the comparator molecules (ascorbic acid, resveratrol, and trolox). Only three compounds (, , ) yielded modest AChE/BuChE inhibitions (>10%). Please note that a SciFinder substance data base search confirmed that most of the compounds reported herein are new, except and which are also commercially available.

A Fast and Validated Reversed-Phase HPLC Method for Simultaneous Determination of Simvastatin, Atorvastatin, Telmisartan and Irbesartan in Bulk Drugs and Tablet Formulations.

Alhazmi HA, Alnami AM, Arishi MAA … +5 more , Alameer RK, Al Bratty M, Rehman ZU, Javed SA, Arbab IA

Sci Pharm · 2017 Dec · PMID 29257120 · Full text

The aim of this study was to develop and validate a fast and simple reversed-phase HPLC method for simultaneous determination of four cardiovascular agents-atorvastatin, simvastatin, telmisartan and irbesartan in bulk dr... The aim of this study was to develop and validate a fast and simple reversed-phase HPLC method for simultaneous determination of four cardiovascular agents-atorvastatin, simvastatin, telmisartan and irbesartan in bulk drugs and tablet oral dosage forms. The chromatographic separation was accomplished by using Symmetry C18 column (75 mm × 4.6 mm; 3.5 μ) with a mobile phase consisting of ammonium acetate buffer (10 mM; pH 4.0) and acetonitrile in a ratio 40:60 /. Flow rate was maintained at 1 mL/min up to 3.5 min, and then suddenly changed to 2 mL/min till the end of the run (7.5 min). The data was acquired using ultraviolet detector monitored at 220 nm. The method was validated for linearity, precision, accuracy and specificity. The developed method has shown excellent linearity (R² > 0.999) over the concentration range of 1-16 µg/mL. The limits of detection (LODs) and limits of quantification (LOQs) were in the range of 0.189-0.190 and 0.603-0.630 µg/mL, respectively. Inter-day and intra-day accuracy and precision data were recorded in the acceptable limits. The new method has successfully been applied for quantification of all four drugs in their tablet dosage forms with percent recovery within 100 ± 2%.

Theoretical Investigation of the Enantioselective Complexations between pfDHFR and Cycloguanil Derivatives.

Kulatee S, Toochinda P, Suksangpanomrung A … +1 more , Lawtrakul L

Sci Pharm · 2017 Nov · PMID 29160825 · Full text

Point mutations in dihydrofolate reductase (DHFR), especially the double mutant variant (A16V + S108T), led to ineffective inhibiting by cycloguanil (Cyc). Cycloguanil derivatives showed good inhibiting properties again... Point mutations in dihydrofolate reductase (DHFR), especially the double mutant variant (A16V + S108T), led to ineffective inhibiting by cycloguanil (Cyc). Cycloguanil derivatives showed good inhibiting properties against wild-type and mutant DHFR with an inhibition constant as low as the nanomolar level. However, there have been no reports on the stereochemistry of the compounds, and this is important because the pure enantiomeric form of a chiral drug can exert desirable, as well as non-desirable responses on the body or both. In this work, three-dimensional structures of Cyc derivatives in and configuration were constructed and optimized using Hartree-Fock/6-31G (d,p). Their structures were docked into the binding pocket of wild-type and double mutant (A16V + S108T) DHFR, complexed with nicotinamide adenine dinucleotide phosphate (NADPH). Results indicate that both wild-type and mutant DHFR are enantioselective towards enantiomeric Cyc derivatives ( and configuration).

Leishmanicidal Activity of Biogenic Fe₃O₄ Nanoparticles.

Khatami M, Alijani H, Sharifi I … +5 more , Sharifi F, Pourseyedi S, Kharazi S, Lima Nobre MA, Khatami M

Sci Pharm · 2017 Nov · PMID 29156612 · Full text

Due to the multiplicity of useful applications of metal oxide nanoparticles (ONPs) in medicine are growing exponentially, in this study, Fe₃O₄ (iron oxide) nanoparticles (IONPs) were biosynthesized using Rosemary to eval... Due to the multiplicity of useful applications of metal oxide nanoparticles (ONPs) in medicine are growing exponentially, in this study, Fe₃O₄ (iron oxide) nanoparticles (IONPs) were biosynthesized using Rosemary to evaluate the leishmanicidal efficiency of green synthesized IONPs. This is the first report of the leishmanicidal efficiency of green synthesized IONPs against The resulting biosynthesized IONPs were characterized by ultraviolet-visible spectroscopy (UV-Vis), X-ray diffraction (XRD), transmission electron microscopy (TEM), and Fourier transform infrared spectroscopy (FTIR). The leishmanicidal activity of IONPS was studied via 3-4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The results showed the fabrication of the spherical shape of monodisperse IONPs with a size 4 ± 2 nm. The UV-visible spectrophotometer absorption peak was at 334 nm. The leishmanicidal activity of biogenic iron oxide nanoparticles against (promastigote) was also studied. The IC of IONPs was 350 µg/mL. In this report, IONPs were synthesized via a green method. IONPs are mainly spherical and homogeneous, with an average size of about 4 nm, and were synthesized here using an eco-friendly, simple, and inexpensive method.

Hydrogen Sulfide Releasing 2-Mercaptoacrylic Acid-Based Derivative Possesses Cytoprotective Activity in a Small Intestine of Rats with Medication-Induced Enteropathy.

Sklyarova Y, Fomenko I, Lozynska I … +3 more , Lozynskyi A, Lesyk R, Sklyarov A

Sci Pharm · 2017 Oct · PMID 29064425 · Full text

Small intestinal injury is known to be one of the most commonly appearing pathologies, resulting in the use of medications such as: nonsteroidal anti-inflammatory drugs (NSAIDs), antitumor drugs and angiotensin-convertin... Small intestinal injury is known to be one of the most commonly appearing pathologies, resulting in the use of medications such as: nonsteroidal anti-inflammatory drugs (NSAIDs), antitumor drugs and angiotensin-converting enzyme (ACE) inhibitors. The principal objective of this study is to evaluate the action of a novel mercaptoacrylic acid derivative able to release H₂S on parameters of NO-synthase system and oxidative stress. Inducing enteropathy, three types of medications were used: indomethacin, an NSAID (35 mg/kg); methotrexate, an antitumor drug (10 mg/kg); and enalapril, an ACE inhibitor (2 mg/kg/day). 2-[(4-chlorophenyl-carbamoyl)-methyl]-3-(3,5-di-tert-butyl-4-hydroxyphenyl)-acrylic acid (2C3DHTA) was introduced based on the background of medication-induced enteropathy (10 mg/kg/day). The survey showed that malondialdehyde (MDA) concentration, myeloperoxidase (MPO) activity, superoxide dismutase (SOD), catalase, and NO-synthases (NOS) were determined in the small intestinal mucosa. The increase in inducible NO-synthase (iNOS) activity was due to indomethacin and methotrexate administration. Constitutive NO-synthase (cNOS) activity was decreased by an ACE-inhibitor. The cytoprotective effect was demonstrated by 2C3DHTA, which returned iNOS activity to its control level and increased cNOS activity. The enterotoxic action of studied medication was accompanied by the development of oxidative stress manifested, activity of MPO was increased. MPO activity and manifestations of oxidative stress were decreased by 2C3DHTA. Effects of 2C3DHTA can be explained by the action of H₂S, released from this compound in the gastrointestinal (GI) system.

Antimycobacterial Activities of N-Substituted-Glycinyl 1H-1,2,3-Triazolyl Oxazolidinones and Analytical Method Development and Validation for a Representative Compound.

Al-Tannak NF, Phillips OA

Sci Pharm · 2017 Oct · PMID 28974052 · Full text

Twelve -substituted-glycinyl triazolyl oxazolidinone derivatives were screened for antimycobacterial activity against susceptible ( ( H37Rv) and resistant (isoniazid (INH)-resistant (SRI 1369), rifampin (RMP)-resistant... Twelve -substituted-glycinyl triazolyl oxazolidinone derivatives were screened for antimycobacterial activity against susceptible ( ( H37Rv) and resistant (isoniazid (INH)-resistant (SRI 1369), rifampin (RMP)-resistant (SRI 1367), and ofloxacin (OFX)-resistant (SRI 4000)) strains. Most of the compounds showed moderate to strong antimycobacterial activity against all strains tested, with minimum inhibitory concentration (MIC) value ranges of 0.5-11.5, 0.056-11.6, 0.11-5.8, and 0.03-11.6 μM, and percent inhibition ranges of 41-79%, 51-72%, 50-75%, and 52-71% against H37Rv, INH-R, RMP-R, and OFX-R , respectively. The 3,5-dinitrobenzoyl and 5-nitrofuroyl derivatives demonstrated strong antimycobacterial activities with the -(5-nitrofuroyl) derivatives ( and ) being the most potent, with MIC value range of 0.3-0.6 μM against all strains tested. Compounds were not bactericidal, but showed intracellular (macrophage) antimycobacterial activity. A reliable validated analytical method was developed for a representative compound using Waters Acquity ultra High-Performance Liquid Chromatography (UHPLC) system with quaternary Solvent Manager (H-Class). A simple extraction method indicated that was stable in human plasma after 90 min at 37 °C with more than 90% successfully recovered. Moreover, stress stability studies were performed and degradants were identified by using UHPLC-ESI-QToF under acidic, basic, and oxidative simulated conditions.

A Review of the Composition of the Essential Oils and Biological Activities of Angelica Species.

Sowndhararajan K, Deepa P, Kim M … +2 more , Park SJ, Kim S

Sci Pharm · 2017 Sep · PMID 28930168 · Full text

A number of species have been used in traditional systems of medicine to treat many ailments. Especially, essential oils (EOs) from the species have been used for the treatment of various health problems, including mal... A number of species have been used in traditional systems of medicine to treat many ailments. Especially, essential oils (EOs) from the species have been used for the treatment of various health problems, including malaria, gynecological diseases, fever, anemia, and arthritis. EOs are complex mixtures of low molecular weight compounds, especially terpenoids and their oxygenated compounds. These components deliver specific fragrance and biological properties to essential oils. In this review, we summarized the chemical composition and biological activities of EOs from different species of . For this purpose, a literature search was carried out to obtain information about the EOs of species and their bioactivities from electronic databases such as PubMed, Science Direct, Wiley, Springer, ACS, Google, and other journal publications. There has been a lot of variation in the EO composition among different species. EOs from species were reported for different kinds of biological activities, such as antioxidant, anti-inflammatory, antimicrobial, immunotoxic, and insecticidal activities. The present review is an attempt to consolidate the available data for different species on the basis of major constituents in the EOs and their biological activities.

In Vitro Activities of Enantiopure and Racemic 1'-Acetoxychavicol Acetate against Clinical Isolates of Mycobacterium tuberculosis.

Warit S, Rukseree K, Prammananan T … +8 more , Hongmanee P, Billamas P, Jaitrong S, Chaiprasert A, Jaki BU, Pauli GF, Franzblau SG, Palittapongarnpim P

Sci Pharm · 2017 Sep · PMID 28927024 · Full text

In the process of evaluating the effect of several plant extracts against using the Microplate Alamar Blue Assay (MABA), an extract of Thai herb rhizome and its major component, 1'-acetoxychavicol acetate (ACA), exhibi... In the process of evaluating the effect of several plant extracts against using the Microplate Alamar Blue Assay (MABA), an extract of Thai herb rhizome and its major component, 1'-acetoxychavicol acetate (ACA), exhibited marked anti-tuberculosis activity. The minimal inhibition concentrations (MICs) of the -enantiomer of ACA (-ACA) against H37R ATCC 25177 and H37R ATCC 27294 strains were 0.2 µg/mL and 0.7 µg/mL, respectively. More than 95% of 100 drug-sensitive and 50 drug-resistant mycobacterial clinical isolates were inhibited by extracted -ACA at 1.0 µg/mL. All of the remaining isolates were inhibited at 2.0 µg/mL. In contrast to the -enantiomer, synthetic racemic 1'--ACA (-ACA) showed MICs of 0.5 µg/mL and 2.7 µg/mL for H37R ATCC 25177 and H37R ATCC 27294, respectively, suggesting that the anti-tuberculosis effect might be primarily due to the -form. These observations were in line with the MICs of -ACA against 98% of 93 drug-resistant clinical isolates, which showed the effective inhibitory dose at 2.0 µg/mL. After exposure to 2.7 µg/mL of -ACA for at least 3 h, the tubercle bacilli were completely killed. These demonstrated that ACA had potent anti-TB activity.

Structural and Dynamics Perspectives on the Binding of Substrate and Inhibitors in Mycobacterium tuberculosis DHFR.

Sittikornpaiboon P, Toochinda P, Lawtrakul L

Sci Pharm · 2017 Sep · PMID 28914808 · Full text

Dihydrofolate reductase (DHFR), an essential enzyme in the folate pathway, is a potential target for new anti-tuberculosis drugs. Fifteen crystal structures of DHFR complexed with NADPH and various inhibitors are availa... Dihydrofolate reductase (DHFR), an essential enzyme in the folate pathway, is a potential target for new anti-tuberculosis drugs. Fifteen crystal structures of DHFR complexed with NADPH and various inhibitors are available in the RCSB Protein Data Bank, but none of them is a substrate binding structure. Therefore, we performed molecular dynamics simulations on ternary complexes of DHFR:NADPH with a substrate (dihydrofolate) and each of three competitive inhibitors the in 2,4-diaminopyrimidine series (P1, P157, and P169), in order to gain insight into the inhibition-mechanism of DHFR in the folate pathway. The binding energy and thermodynamics values of each system were calculated by the Molecular Mechanics/Generalized Born Surface Area (MM/GBSA) method. The dynamics of the enzyme and the motion of each amino acid residue at the active site were examined. The key factors that promote the binding of P157 and P169 on DHFR (mtbDHFR) reveal opportunities for using these compounds as novel anti-tuberculosis drugs.

ALKALOIDS FROM OXYTROPIS MYRIOPHYLLA (PALL) DC.

Kojima K, S P, S N … +4 more , S T, Ya J, Lsaka K, Ogihara Y

Sci Pharm · 2017 Aug · PMID 28841190 · Publisher ↗

Five alkaloids were isolated from the epigeal part of Oxytropis myriophylla. Three alkaloids were identified as N-benzoyl-β-phenylethylamine, N-trans-cinnamoyl-β-phenylethylamine, N-cis-cinnamoyl-β-phenylethylamine and t... Five alkaloids were isolated from the epigeal part of Oxytropis myriophylla. Three alkaloids were identified as N-benzoyl-β-phenylethylamine, N-trans-cinnamoyl-β-phenylethylamine, N-cis-cinnamoyl-β-phenylethylamine and the structures of two new alkaloids were elucidated to be N-benzoyl-β-hydroxyphenylethylarnine(2), N-trans-cinnamoyl-β-hydroxy-phenylethylamine(5). The absolu.te structures were established by modified Mosher method.

Zytoprotektion mit Amifostin (Ethyol) in der Chemotherapie: Meta-Analyse zum pharmakokinetischen Interaktionspotential mit Zytostatika.

Czejka M, Schüller J, Kletzl H

Sci Pharm · 2017 Aug · PMID 28841172 · Publisher ↗

The cytoprotective agent amifostine (AMI) is capable to protect healthy cells (contrary to tumor cells) due to higher activity of alkaline phosphatase at the membrane site of normal cells. In seven clinical trials the in... The cytoprotective agent amifostine (AMI) is capable to protect healthy cells (contrary to tumor cells) due to higher activity of alkaline phosphatase at the membrane site of normal cells. In seven clinical trials the influence of AMI on the pharmacokinetics of different cytostatics was investigated. Preadministration of AMI increased Cmax of doxorubicin (+ 44 %, p < 0.06), epirubicin (+ 31 %, P < 0.08), mitomycin C (+ 41 %, p < 0.01) and docetaxel (+ 31 % and + 17 %, not significant). In contrary, the peak concentration of pirarubicin , the tetrahydropyranyl-prodrug of doxorubicin was decreased (- 50 %, P < 0.03), leading to an equal higher concentrationof doxorubicin in the blood . In accordance to the peak concentrations, the AUC'ast was increased by chemoprotection: doxorubicin + 53 % (p < 0.01) and epirubicin + 23 % (not significant), docetaxel + 25 % and + 31 % (not significant). AUC'ast of mitomycin C and paclitaxel seemed to be unaffected by preadministered AMI. A particular inhibition of the protein binding by AMI has been identified as one reason for higher serum concentrations of anthracycline drugs. After cytoprotection, a possible increase of the cytostatic's Serum concentrations should be taken into account for optimal dosage schedules.

Evaluation of Acute and Subacute Oral Toxicity Induced by Ethanolic Extract of Marsdenia tenacissima Leaves in Experimental Rats.

Porwal M, Khan NA, Maheshwari KK

Sci Pharm · 2017 Aug · PMID 28825665 · Full text

The objective of this study is to evaluate the acute and subacute toxicity of the ethanolic extract of (MTE) leaves (family: Asclepiadaceae) in albino rats. The acute toxicity was performed where the limit dose of 5000... The objective of this study is to evaluate the acute and subacute toxicity of the ethanolic extract of (MTE) leaves (family: Asclepiadaceae) in albino rats. The acute toxicity was performed where the limit dose of 5000 mg/kg body weight used. Observations were made and recorded for 24 h, and once daily further for a period of 14 days. The rats were weighed and various observations, like mortality, behavior, injury, or any signs of illness were conducted once daily during the period. For subacute study, four groups of 10 animals (female rats) received 10% Tween 20 in distilled water (control), and 250, 500, and 1000 mg/kg of freshly-prepared extracts, respectively, every 24 h orally for 28 days. At the end of each study, hematological analysis and biochemical parameters were evaluated. Histopathological examination of vital organs of the animals were taken for gross findings, compared to controls. There was no significant difference ( > 0.05) observed in the relative organs, body weights, hematological, biochemical parameters, and gross abnormalities, compared to the control. No mortality was recorded. Therefore, analysis of results may lead to the conclusion that the medium-term oral administration of the MTE leaves for 28 days does not cause toxicity.

Extractive Spectrophotometric Determination of Nortriptyline Hydrochloride Using Sudan II, IV and Black B.

Amin AS, Saleh HM

Sci Pharm · 2017 Aug · PMID 28817110 · Publisher ↗

A simple spectrophotometric methods has been developed for the determination of nortriptyline hydrochloride in pure and in pharmaceuticalformulations based on the formation of ion-pair complexes with sudun II (S), sudan... A simple spectrophotometric methods has been developed for the determination of nortriptyline hydrochloride in pure and in pharmaceuticalformulations based on the formation of ion-pair complexes with sudun II (S), sudan (IV) (S) and sudan black B (S). The selectivity of the method was improved through extraction with chloroform. The optimum conditions for complete extracted colour development were assessed. The absorbance measurements were made at 534, 596 and 649 nm for S, S and S complexes, respectively. The calibration graph was linear in the ranges 0.5- 280. 0.5- 37.5 and 0.5 - 31.0 μg ml of the drug usiny the same reagents, respectively. The precision of the procedure was checked by calculating the relative standard deviation of ten replicate determinations on 15 μg ml of nortriptyline HCI and was found to be 1.7, 1.3 and 1.55% using S, S, and S complexes, respectively. The molar absorptivity and Sandell sensitivity for each ion-pair were calculated. The proposed methods were successfully applied to the deterniination of pure nortriptyline HCI and in pharmaceutical formulations, and the results demonstrated that the method is equally accurate, precise and reproducible as the official method.

Diterpenoid Alkaloids from Consolida regalis S. F.Gray subsp.paniculata (Host) Soo var. paniculata.

Mericl F, Mericli AH, Desai HK … +2 more , Ulubelen A, Pelletier SW

Sci Pharm · 2017 Aug · PMID 28813032 · Publisher ↗

Seven diterpenoid alkaloids : delcosine(1), delsoline(2), gigactonine(3), lycoctonine(4), takaosamine(5), atisine(6) and hetisinone(7) have been isolated from the aerial parts of Consolida regalis subsp. paniculata var.... Seven diterpenoid alkaloids : delcosine(1), delsoline(2), gigactonine(3), lycoctonine(4), takaosamine(5), atisine(6) and hetisinone(7) have been isolated from the aerial parts of Consolida regalis subsp. paniculata var. paniculata. The presence of compounds 1,2,5,6 and 7 in this plant has not been previously reported.

Determination of Amineptine and Amprolium Hydrochlorides through Ion Associates with Cobalt (II) Thiocyanate.

Fekria M AA

Sci Pharm · 2017 Aug · PMID 28809815 · Publisher ↗

Two new methods for the determination of amineptine (AMN) and amprolium (AMP) have been developed. The methods consist of extractin the ion - pairs between the drug and the inorganic complex [Co (SCN)₄]. The optimal expe... Two new methods for the determination of amineptine (AMN) and amprolium (AMP) have been developed. The methods consist of extractin the ion - pairs between the drug and the inorganic complex [Co (SCN)₄]. The optimal experimental conditions of both methods including pH, concentration of Co (II) and tlxocyanate ions, and the organic solvents were studied. The optimum pH was found to be 3.9, nitrobenzene proved to be the most suitable solvent, giving quantitative extraction for the two drugs. The two drugs can be determined in the organic phase spectrophotometrically at 625 nm showing Sandell sensitivities of 0.19 and 0.12 µg cm with relative standard deviation of 0.46 and 0.87 % for amineptine and amprolium, respectively.The indirect method was also applied to measure cobalt in the organic phase by atomic absorption spectrometry at 240.7 nm, and the relative standard deviation of the method is approximately 0.35 and 0.29 % for amineptine and amprolium, respectively. The proposed methods were found to be suitable for the accurate, simple and rapid analysis of amineptine and amprolium hydrochlorides in the bulk drugs and in pharmaceutical forms.
← Prev Page 3 of 10 Next →

About

Frequency
Sun
Papers found
200
RSS feed
Subscribe